Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AGI-5198 (IDH-C35) 是一种选择性的突变体 IDH1R132H 抑制剂,IC50=0.07 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 297 | 现货 | ||
10 mg | ¥ 493 | 现货 | ||
50 mg | ¥ 726 | 现货 | ||
100 mg | ¥ 1,190 | 现货 | ||
200 mg | ¥ 1,960 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 541 | 现货 |
产品描述 | AGI-5198 (IDH-C35) is a highly effective and specific inhibitor of IDH1 R132H/R132C mutants (IC50: 0.07/0.16 μM). |
靶点活性 | R132H-IDH1:70 nM, R132C-IDH1:0.16 μM |
体外活性 | 在带有Ki-67蛋白抗体染色的小鼠体内,AGI-5198可使其肿瘤减少.但空白对照组和AGI-5198处理组的小鼠肿瘤中裂解的caspase-3无显著差异.AGI-5198(450 mg/kg/day)治疗R132H-IDH1胶质瘤移植瘤三周,可抑制50-60%的生长,但不影响IDH1野生型胶质瘤移植瘤的生长. |
体内活性 | AGI-5198对TS603胶质瘤细胞系有一定抗肿瘤疗效,且剂量依赖性抑制R-2HG产生。在R-2HG几乎被完全抑制的条件下,AGI-5198对组蛋白H3K9me3去甲基化有诱导作用,且诱导与胶质基因分化相关的基因表达。在全基因组DNA甲基化中,AGI-5198对mIDH1受损的IDH1突变型生长具有抑制作用,但野生型生长几乎没有受到影响。AGI-5198对突变型IDH1(R132H-IDH1 和 R132C-IDH1)有明显抑制作用,但对野生型IDH1 (IC50>100 μM) 或任何IDH2亚型(R140Q, R172K, 野生型) (IC50>100 μM)抑制作用非常弱。 |
激酶实验 | IDH enzyme activity: Compound is prepared as 10 mM stock in DMSO and diluted to 50X final concentration in DMSO, for a 50 μL reaction mixture. IDH enzyme activity converting alpha-ketogluta rate to 2-hydroxyglutarate is measured using a NADPH depletion assay. In the assay the remaining cofactor is measured at the end of the reaction with the addition of a catalytic excess of diaphorase and resazurin, to generate a fluorescent signal in proportion to the amount of NADPH remaining. IDH enzyme activity in the direction of isocitrate to alpha-ketoglutarate conversion is measured by direct coupling of the NADPH production to conversion of resazurin to resorufin by diaphorase. In both cases, resorufin is measured fluorometrically at Ex544 Em 590. |
细胞实验 | AGI-5198 is dissolved in DMSO.TS603 cells are grown in medium containing either AGI-5198 (1.5 μM) or DMSO vehicle control.One week prior to harvest cells are ransferred to differentiation medium (DMEM F12; 15 mM HEPES; 0.06% glucose; B27 without vitamin A; N2; Insulin/transferrin; 1% FBS) containing freshly added retinoic acid (1 μM).ChIP of non-crosslinked cells is then carried out using established ChIP methods.350 μg of lysate is immunoprecipitated-using anti-H3K9Me3,H3K27me3 or Rabbit Control IgG.After washing,ChIP DNA is eluted from protein G beads and analyzed by RT-PCR using SYBR green.Relative occupancy is calculated using the standard curve method and fold enrichment versus IgG.Enrichment in AGI- 5198-treated cells is normalized to vehicle control.Means and standard deviation are calculated from 4 technical replicates. |
别名 | IDH-C35 |
分子量 | 462.56 |
分子式 | C27H31FN4O2 |
CAS No. | 1355326-35-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 23 mg/mL (49.7 mM)
Ethanol: 12 mg/mL (25.9 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.1619 mL | 10.8094 mL | 21.6188 mL | 54.047 mL |
5 mM | 0.4324 mL | 2.1619 mL | 4.3238 mL | 10.8094 mL | |
10 mM | 0.2162 mL | 1.0809 mL | 2.1619 mL | 5.4047 mL | |
20 mM | 0.1081 mL | 0.5405 mL | 1.0809 mL | 2.7024 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
AGI-5198 1355326-35-0 Metabolism Dehydrogenase Isocitrate Dehydrogenase (IDH) Inhibitor inhibit AGI 5198 AGI5198 IDH-C35 inhibitor